Assay Detail

CHEMBL4016576

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Binding

Inhibition of PI3Kgamma (unknown origin) after 60 mins using fluorescein-labeled kinase tracer by HTRF assay

ChEMBL ↗

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Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) ↗

Open DB target context

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Loading context

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

CHEMBL3267

Anchored from Assay target.

Protein identity Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.
J Med Chem (2017) 60 : 5193 -5208
PubMed 28541707 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.39	7.39

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4064666	—	—	1	7.39

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4064666	—	IC50	=	41.0	nM	7.39